US6248310B1 - Anti-tartar dental product and method - Google Patents
Anti-tartar dental product and method Download PDFInfo
- Publication number
- US6248310B1 US6248310B1 US09/538,564 US53856400A US6248310B1 US 6248310 B1 US6248310 B1 US 6248310B1 US 53856400 A US53856400 A US 53856400A US 6248310 B1 US6248310 B1 US 6248310B1
- Authority
- US
- United States
- Prior art keywords
- composition
- phosphate
- calcium
- sodium
- weight
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 208000006558 Dental Calculus Diseases 0.000 title claims abstract description 28
- 238000000034 method Methods 0.000 title claims abstract description 13
- 229940023487 dental product Drugs 0.000 title claims description 4
- 239000000203 mixture Substances 0.000 claims abstract description 122
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 33
- 239000000463 material Substances 0.000 claims abstract description 20
- 150000003013 phosphoric acid derivatives Chemical class 0.000 claims abstract description 18
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims abstract description 17
- 239000011575 calcium Substances 0.000 claims abstract description 15
- 229910052791 calcium Inorganic materials 0.000 claims abstract description 15
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims abstract description 14
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 claims abstract description 8
- MHAJPDPJQMAIIY-UHFFFAOYSA-N Hydrogen peroxide Chemical compound OO MHAJPDPJQMAIIY-UHFFFAOYSA-N 0.000 claims description 22
- 239000001506 calcium phosphate Substances 0.000 claims description 22
- 235000011010 calcium phosphates Nutrition 0.000 claims description 13
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 12
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 12
- 229910019142 PO4 Inorganic materials 0.000 claims description 11
- XEFQLINVKFYRCS-UHFFFAOYSA-N Triclosan Chemical compound OC1=CC(Cl)=CC=C1OC1=CC=C(Cl)C=C1Cl XEFQLINVKFYRCS-UHFFFAOYSA-N 0.000 claims description 11
- 229910000389 calcium phosphate Inorganic materials 0.000 claims description 11
- 239000010452 phosphate Substances 0.000 claims description 10
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims description 9
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 9
- 229960003500 triclosan Drugs 0.000 claims description 8
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 6
- 230000000675 anti-caries Effects 0.000 claims description 6
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims description 6
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims description 6
- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 6
- 239000001488 sodium phosphate Substances 0.000 claims description 5
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims description 4
- 239000001110 calcium chloride Substances 0.000 claims description 4
- 229910001628 calcium chloride Inorganic materials 0.000 claims description 4
- 235000011148 calcium chloride Nutrition 0.000 claims description 4
- 159000000007 calcium salts Chemical class 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 claims description 4
- -1 fluoride compound Chemical class 0.000 claims description 4
- 239000004254 Ammonium phosphate Substances 0.000 claims description 3
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 3
- 206010044029 Tooth deposit Diseases 0.000 claims description 3
- 229910000148 ammonium phosphate Inorganic materials 0.000 claims description 3
- 235000019289 ammonium phosphates Nutrition 0.000 claims description 3
- 230000001680 brushing effect Effects 0.000 claims description 3
- VSGNNIFQASZAOI-UHFFFAOYSA-L calcium acetate Chemical compound [Ca+2].CC([O-])=O.CC([O-])=O VSGNNIFQASZAOI-UHFFFAOYSA-L 0.000 claims description 3
- 235000011092 calcium acetate Nutrition 0.000 claims description 3
- 239000001639 calcium acetate Substances 0.000 claims description 3
- 229960005147 calcium acetate Drugs 0.000 claims description 3
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 3
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical group [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims description 3
- BRPQOXSCLDDYGP-UHFFFAOYSA-N calcium oxide Chemical compound [O-2].[Ca+2] BRPQOXSCLDDYGP-UHFFFAOYSA-N 0.000 claims description 3
- 239000000292 calcium oxide Substances 0.000 claims description 3
- ODINCKMPIJJUCX-UHFFFAOYSA-N calcium oxide Inorganic materials [Ca]=O ODINCKMPIJJUCX-UHFFFAOYSA-N 0.000 claims description 3
- 239000001175 calcium sulphate Substances 0.000 claims description 3
- 235000011132 calcium sulphate Nutrition 0.000 claims description 3
- MNNHAPBLZZVQHP-UHFFFAOYSA-N diammonium hydrogen phosphate Chemical compound [NH4+].[NH4+].OP([O-])([O-])=O MNNHAPBLZZVQHP-UHFFFAOYSA-N 0.000 claims description 3
- CUXQLKLUPGTTKL-UHFFFAOYSA-M microcosmic salt Chemical compound [NH4+].[Na+].OP([O-])([O-])=O CUXQLKLUPGTTKL-UHFFFAOYSA-M 0.000 claims description 3
- 239000011736 potassium bicarbonate Substances 0.000 claims description 3
- 235000015497 potassium bicarbonate Nutrition 0.000 claims description 3
- 229910000028 potassium bicarbonate Inorganic materials 0.000 claims description 3
- 229910000027 potassium carbonate Inorganic materials 0.000 claims description 3
- 235000011181 potassium carbonates Nutrition 0.000 claims description 3
- TYJJADVDDVDEDZ-UHFFFAOYSA-M potassium hydrogencarbonate Chemical compound [K+].OC([O-])=O TYJJADVDDVDEDZ-UHFFFAOYSA-M 0.000 claims description 3
- 229910000162 sodium phosphate Inorganic materials 0.000 claims description 3
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 claims description 3
- 150000007522 mineralic acids Chemical class 0.000 claims description 2
- 150000003751 zinc Chemical class 0.000 claims 2
- FNAQSUUGMSOBHW-UHFFFAOYSA-H calcium citrate Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O FNAQSUUGMSOBHW-UHFFFAOYSA-H 0.000 claims 1
- 239000001354 calcium citrate Substances 0.000 claims 1
- 235000013337 tricalcium citrate Nutrition 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 abstract description 6
- 230000002401 inhibitory effect Effects 0.000 abstract description 3
- 239000013588 oral product Substances 0.000 abstract 1
- 229940023486 oral product Drugs 0.000 abstract 1
- 239000000047 product Substances 0.000 abstract 1
- 239000006072 paste Substances 0.000 description 23
- 239000000499 gel Substances 0.000 description 21
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 description 18
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 16
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 16
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 14
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 14
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 13
- 229960005069 calcium Drugs 0.000 description 12
- 239000000796 flavoring agent Substances 0.000 description 11
- 235000019634 flavors Nutrition 0.000 description 11
- LRCFXGAMWKDGLA-UHFFFAOYSA-N dioxosilane;hydrate Chemical compound O.O=[Si]=O LRCFXGAMWKDGLA-UHFFFAOYSA-N 0.000 description 10
- 229960004029 silicic acid Drugs 0.000 description 10
- 239000011775 sodium fluoride Substances 0.000 description 10
- 235000013024 sodium fluoride Nutrition 0.000 description 10
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 9
- 239000004141 Sodium laurylsulphate Substances 0.000 description 9
- 239000001768 carboxy methyl cellulose Substances 0.000 description 9
- 235000021317 phosphate Nutrition 0.000 description 9
- 235000017557 sodium bicarbonate Nutrition 0.000 description 9
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 9
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 9
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 8
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 8
- 235000019441 ethanol Nutrition 0.000 description 8
- 235000011187 glycerol Nutrition 0.000 description 8
- 239000004615 ingredient Substances 0.000 description 8
- 235000019691 monocalcium phosphate Nutrition 0.000 description 8
- 229910000150 monocalcium phosphate Inorganic materials 0.000 description 8
- 229920005862 polyol Polymers 0.000 description 8
- 230000009467 reduction Effects 0.000 description 8
- 239000000600 sorbitol Substances 0.000 description 8
- 235000010356 sorbitol Nutrition 0.000 description 8
- 239000000606 toothpaste Substances 0.000 description 8
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 7
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 7
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 7
- YYRMJZQKEFZXMX-UHFFFAOYSA-L calcium bis(dihydrogenphosphate) Chemical compound [Ca+2].OP(O)([O-])=O.OP(O)([O-])=O YYRMJZQKEFZXMX-UHFFFAOYSA-L 0.000 description 7
- ZBZJARSYCHAEND-UHFFFAOYSA-L calcium;dihydrogen phosphate;hydrate Chemical compound O.[Ca+2].OP(O)([O-])=O.OP(O)([O-])=O ZBZJARSYCHAEND-UHFFFAOYSA-L 0.000 description 7
- 229940041616 menthol Drugs 0.000 description 7
- 229940100474 polyethylene glycol 1450 Drugs 0.000 description 7
- 150000003077 polyols Chemical class 0.000 description 7
- ILJOYZVVZZFIKA-UHFFFAOYSA-M sodium;1,1-dioxo-1,2-benzothiazol-3-olate;hydrate Chemical compound O.[Na+].C1=CC=C2C(=O)[N-]S(=O)(=O)C2=C1 ILJOYZVVZZFIKA-UHFFFAOYSA-M 0.000 description 7
- 239000004408 titanium dioxide Substances 0.000 description 7
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 6
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 6
- 238000009472 formulation Methods 0.000 description 6
- 229910052588 hydroxylapatite Inorganic materials 0.000 description 6
- XYJRXVWERLGGKC-UHFFFAOYSA-D pentacalcium;hydroxide;triphosphate Chemical compound [OH-].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O XYJRXVWERLGGKC-UHFFFAOYSA-D 0.000 description 6
- 229920001992 poloxamer 407 Polymers 0.000 description 6
- 238000012360 testing method Methods 0.000 description 6
- 229940034610 toothpaste Drugs 0.000 description 6
- 239000003795 chemical substances by application Substances 0.000 description 5
- 238000002156 mixing Methods 0.000 description 5
- 229920001223 polyethylene glycol Polymers 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- 239000004094 surface-active agent Substances 0.000 description 5
- SGHZXLIDFTYFHQ-UHFFFAOYSA-L Brilliant Blue Chemical compound [Na+].[Na+].C=1C=C(C(=C2C=CC(C=C2)=[N+](CC)CC=2C=C(C=CC=2)S([O-])(=O)=O)C=2C(=CC=CC=2)S([O-])(=O)=O)C=CC=1N(CC)CC1=CC=CC(S([O-])(=O)=O)=C1 SGHZXLIDFTYFHQ-UHFFFAOYSA-L 0.000 description 4
- 239000004161 brilliant blue FCF Substances 0.000 description 4
- 235000012745 brilliant blue FCF Nutrition 0.000 description 4
- 238000011156 evaluation Methods 0.000 description 4
- 239000003906 humectant Substances 0.000 description 4
- 150000002978 peroxides Chemical class 0.000 description 4
- 239000002562 thickening agent Substances 0.000 description 4
- 239000003082 abrasive agent Substances 0.000 description 3
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 3
- 229920006318 anionic polymer Polymers 0.000 description 3
- 150000007942 carboxylates Chemical group 0.000 description 3
- XPPKVPWEQAFLFU-UHFFFAOYSA-J diphosphate(4-) Chemical class [O-]P([O-])(=O)OP([O-])([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-J 0.000 description 3
- 235000011180 diphosphates Nutrition 0.000 description 3
- 229920000642 polymer Polymers 0.000 description 3
- 239000000377 silicon dioxide Substances 0.000 description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 3
- FQENQNTWSFEDLI-UHFFFAOYSA-J sodium diphosphate Chemical class [Na+].[Na+].[Na+].[Na+].[O-]P([O-])(=O)OP([O-])([O-])=O FQENQNTWSFEDLI-UHFFFAOYSA-J 0.000 description 3
- WGIWBXUNRXCYRA-UHFFFAOYSA-H trizinc;2-hydroxypropane-1,2,3-tricarboxylate Chemical compound [Zn+2].[Zn+2].[Zn+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O WGIWBXUNRXCYRA-UHFFFAOYSA-H 0.000 description 3
- 235000010493 xanthan gum Nutrition 0.000 description 3
- 239000000230 xanthan gum Substances 0.000 description 3
- 229920001285 xanthan gum Polymers 0.000 description 3
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- 239000011746 zinc citrate Substances 0.000 description 3
- 235000006076 zinc citrate Nutrition 0.000 description 3
- 229940068475 zinc citrate Drugs 0.000 description 3
- 229920002534 Polyethylene Glycol 1450 Polymers 0.000 description 2
- PNEYBMLMFCGWSK-UHFFFAOYSA-N aluminium oxide Inorganic materials [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 description 2
- 230000003610 anti-gingivitis Effects 0.000 description 2
- 229960002713 calcium chloride Drugs 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Natural products OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 2
- 235000015165 citric acid Nutrition 0.000 description 2
- 238000004140 cleaning Methods 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 229920001577 copolymer Polymers 0.000 description 2
- 239000000551 dentifrice Substances 0.000 description 2
- 235000019820 disodium diphosphate Nutrition 0.000 description 2
- GYQBBRRVRKFJRG-UHFFFAOYSA-L disodium pyrophosphate Chemical compound [Na+].[Na+].OP([O-])(=O)OP(O)([O-])=O GYQBBRRVRKFJRG-UHFFFAOYSA-L 0.000 description 2
- 229940038485 disodium pyrophosphate Drugs 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 230000009977 dual effect Effects 0.000 description 2
- 229940091249 fluoride supplement Drugs 0.000 description 2
- UPBDXRPQPOWRKR-UHFFFAOYSA-N furan-2,5-dione;methoxyethene Chemical compound COC=C.O=C1OC(=O)C=C1 UPBDXRPQPOWRKR-UHFFFAOYSA-N 0.000 description 2
- 235000011090 malic acid Nutrition 0.000 description 2
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 2
- 150000004682 monohydrates Chemical class 0.000 description 2
- NROKBHXJSPEDAR-UHFFFAOYSA-M potassium fluoride Chemical compound [F-].[K+] NROKBHXJSPEDAR-UHFFFAOYSA-M 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- 239000003352 sequestering agent Substances 0.000 description 2
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- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 2
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 2
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- 235000019818 tetrasodium diphosphate Nutrition 0.000 description 2
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- LWIHDJKSTIGBAC-UHFFFAOYSA-K tripotassium phosphate Chemical compound [K+].[K+].[K+].[O-]P([O-])([O-])=O LWIHDJKSTIGBAC-UHFFFAOYSA-K 0.000 description 2
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- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 1
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- MOMKYJPSVWEWPM-UHFFFAOYSA-N 4-(chloromethyl)-2-(4-methylphenyl)-1,3-thiazole Chemical compound C1=CC(C)=CC=C1C1=NC(CCl)=CS1 MOMKYJPSVWEWPM-UHFFFAOYSA-N 0.000 description 1
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- 240000004760 Pimpinella anisum Species 0.000 description 1
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- 229920002025 Pluronic® F 88 Polymers 0.000 description 1
- 102000009609 Pyrophosphatases Human genes 0.000 description 1
- 108010009413 Pyrophosphatases Proteins 0.000 description 1
- WINXNKPZLFISPD-UHFFFAOYSA-M Saccharin sodium Chemical compound [Na+].C1=CC=C2C(=O)[N-]S(=O)(=O)C2=C1 WINXNKPZLFISPD-UHFFFAOYSA-M 0.000 description 1
- 239000004965 Silica aerogel Substances 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 235000016639 Syzygium aromaticum Nutrition 0.000 description 1
- 244000223014 Syzygium aromaticum Species 0.000 description 1
- 239000005844 Thymol Substances 0.000 description 1
- 229920001615 Tragacanth Polymers 0.000 description 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- YGCFIWIQZPHFLU-UHFFFAOYSA-N acesulfame Chemical compound CC1=CC(=O)NS(=O)(=O)O1 YGCFIWIQZPHFLU-UHFFFAOYSA-N 0.000 description 1
- 229960005164 acesulfame Drugs 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 150000001252 acrylic acid derivatives Chemical class 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 239000003513 alkali Substances 0.000 description 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 description 1
- 125000000129 anionic group Chemical group 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 239000000605 aspartame Substances 0.000 description 1
- 235000010357 aspartame Nutrition 0.000 description 1
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 1
- 229960003438 aspartame Drugs 0.000 description 1
- YNGQHHUHCOYPKT-UHFFFAOYSA-L azanium;calcium;phosphate Chemical class [NH4+].[Ca+2].[O-]P([O-])([O-])=O YNGQHHUHCOYPKT-UHFFFAOYSA-L 0.000 description 1
- 235000010338 boric acid Nutrition 0.000 description 1
- 125000005619 boric acid group Chemical class 0.000 description 1
- LLSDKQJKOVVTOJ-UHFFFAOYSA-L calcium chloride dihydrate Chemical compound O.O.[Cl-].[Cl-].[Ca+2] LLSDKQJKOVVTOJ-UHFFFAOYSA-L 0.000 description 1
- 229940052299 calcium chloride dihydrate Drugs 0.000 description 1
- WUKWITHWXAAZEY-UHFFFAOYSA-L calcium difluoride Chemical compound [F-].[F-].[Ca+2] WUKWITHWXAAZEY-UHFFFAOYSA-L 0.000 description 1
- JUNWLZAGQLJVLR-UHFFFAOYSA-J calcium diphosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])(=O)OP([O-])([O-])=O JUNWLZAGQLJVLR-UHFFFAOYSA-J 0.000 description 1
- 229910001634 calcium fluoride Inorganic materials 0.000 description 1
- UHHRFSOMMCWGSO-UHFFFAOYSA-L calcium glycerophosphate Chemical compound [Ca+2].OCC(CO)OP([O-])([O-])=O UHHRFSOMMCWGSO-UHFFFAOYSA-L 0.000 description 1
- 229940095618 calcium glycerophosphate Drugs 0.000 description 1
- 235000019299 calcium glycerylphosphate Nutrition 0.000 description 1
- 229910001424 calcium ion Inorganic materials 0.000 description 1
- 229940043256 calcium pyrophosphate Drugs 0.000 description 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical class OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 description 1
- 235000010418 carrageenan Nutrition 0.000 description 1
- 239000000679 carrageenan Substances 0.000 description 1
- 229920001525 carrageenan Polymers 0.000 description 1
- 229940113118 carrageenan Drugs 0.000 description 1
- 125000002091 cationic group Chemical group 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 230000009920 chelation Effects 0.000 description 1
- 150000001860 citric acid derivatives Chemical class 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- GWFAVIIMQDUCRA-UHFFFAOYSA-L copper(ii) fluoride Chemical compound [F-].[F-].[Cu+2] GWFAVIIMQDUCRA-UHFFFAOYSA-L 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 239000000625 cyclamic acid and its Na and Ca salt Substances 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 229940061607 dibasic sodium phosphate Drugs 0.000 description 1
- 235000019821 dicalcium diphosphate Nutrition 0.000 description 1
- NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 description 1
- 229910000390 dicalcium phosphate Inorganic materials 0.000 description 1
- 229940038472 dicalcium phosphate Drugs 0.000 description 1
- CQAIPTBBCVQRMD-UHFFFAOYSA-L dipotassium;phosphono phosphate Chemical compound [K+].[K+].OP(O)(=O)OP([O-])([O-])=O CQAIPTBBCVQRMD-UHFFFAOYSA-L 0.000 description 1
- 229940042400 direct acting antivirals phosphonic acid derivative Drugs 0.000 description 1
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 1
- 229910000397 disodium phosphate Inorganic materials 0.000 description 1
- 235000019800 disodium phosphate Nutrition 0.000 description 1
- CEYULKASIQJZGP-UHFFFAOYSA-L disodium;2-(carboxymethyl)-2-hydroxybutanedioate Chemical compound [Na+].[Na+].[O-]C(=O)CC(O)(C(=O)O)CC([O-])=O CEYULKASIQJZGP-UHFFFAOYSA-L 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- 229960004667 ethyl cellulose Drugs 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 210000002744 extracellular matrix Anatomy 0.000 description 1
- 229910001447 ferric ion Inorganic materials 0.000 description 1
- 229910001448 ferrous ion Inorganic materials 0.000 description 1
- 150000002222 fluorine compounds Chemical class 0.000 description 1
- ZIQLCYCKKROENE-UHFFFAOYSA-L fluoro-dioxido-oxo-$l^{5}-phosphane;tin(2+) Chemical compound [Sn+2].[O-]P([O-])(F)=O ZIQLCYCKKROENE-UHFFFAOYSA-L 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 150000004820 halides Chemical class 0.000 description 1
- 235000001050 hortel pimenta Nutrition 0.000 description 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 229940071826 hydroxyethyl cellulose Drugs 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 235000010494 karaya gum Nutrition 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- ORUIBWPALBXDOA-UHFFFAOYSA-L magnesium fluoride Chemical compound [F-].[F-].[Mg+2] ORUIBWPALBXDOA-UHFFFAOYSA-L 0.000 description 1
- 229910001635 magnesium fluoride Inorganic materials 0.000 description 1
- 239000001630 malic acid Substances 0.000 description 1
- 235000010449 maltitol Nutrition 0.000 description 1
- 239000000845 maltitol Substances 0.000 description 1
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 description 1
- 229940035436 maltitol Drugs 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 229940119047 mentadent Drugs 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 229960001047 methyl salicylate Drugs 0.000 description 1
- XJRBAMWJDBPFIM-UHFFFAOYSA-N methyl vinyl ether Chemical group COC=C XJRBAMWJDBPFIM-UHFFFAOYSA-N 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 229960002900 methylcellulose Drugs 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 235000019426 modified starch Nutrition 0.000 description 1
- 235000016337 monopotassium tartrate Nutrition 0.000 description 1
- 229910000403 monosodium phosphate Inorganic materials 0.000 description 1
- 235000019799 monosodium phosphate Nutrition 0.000 description 1
- 239000002324 mouth wash Substances 0.000 description 1
- 229940051866 mouthwash Drugs 0.000 description 1
- 229920005615 natural polymer Polymers 0.000 description 1
- 150000002823 nitrates Chemical class 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 150000003007 phosphonic acid derivatives Chemical class 0.000 description 1
- 150000003009 phosphonic acids Chemical class 0.000 description 1
- 229920001983 poloxamer Polymers 0.000 description 1
- 229920002503 polyoxyethylene-polyoxypropylene Polymers 0.000 description 1
- 229920001296 polysiloxane Polymers 0.000 description 1
- KYKNRZGSIGMXFH-ZVGUSBNCSA-M potassium bitartrate Chemical compound [K+].OC(=O)[C@H](O)[C@@H](O)C([O-])=O KYKNRZGSIGMXFH-ZVGUSBNCSA-M 0.000 description 1
- 229940081543 potassium bitartrate Drugs 0.000 description 1
- 239000011698 potassium fluoride Substances 0.000 description 1
- 235000003270 potassium fluoride Nutrition 0.000 description 1
- 229910000160 potassium phosphate Inorganic materials 0.000 description 1
- 235000011009 potassium phosphates Nutrition 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 238000009877 rendering Methods 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
- 229940081974 saccharin Drugs 0.000 description 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
- 210000003296 saliva Anatomy 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 229960001462 sodium cyclamate Drugs 0.000 description 1
- 235000019982 sodium hexametaphosphate Nutrition 0.000 description 1
- GCLGEJMYGQKIIW-UHFFFAOYSA-H sodium hexametaphosphate Chemical compound [Na]OP1(=O)OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])O1 GCLGEJMYGQKIIW-UHFFFAOYSA-H 0.000 description 1
- 229940079862 sodium lauryl sarcosinate Drugs 0.000 description 1
- 235000019983 sodium metaphosphate Nutrition 0.000 description 1
- 229960004711 sodium monofluorophosphate Drugs 0.000 description 1
- 235000011008 sodium phosphates Nutrition 0.000 description 1
- 235000019832 sodium triphosphate Nutrition 0.000 description 1
- ADWNFGORSPBALY-UHFFFAOYSA-M sodium;2-[dodecyl(methyl)amino]acetate Chemical compound [Na+].CCCCCCCCCCCCN(C)CC([O-])=O ADWNFGORSPBALY-UHFFFAOYSA-M 0.000 description 1
- HFQQZARZPUDIFP-UHFFFAOYSA-M sodium;2-dodecylbenzenesulfonate Chemical compound [Na+].CCCCCCCCCCCCC1=CC=CC=C1S([O-])(=O)=O HFQQZARZPUDIFP-UHFFFAOYSA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- ANOBYBYXJXCGBS-UHFFFAOYSA-L stannous fluoride Chemical compound F[Sn]F ANOBYBYXJXCGBS-UHFFFAOYSA-L 0.000 description 1
- 229960002799 stannous fluoride Drugs 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000011044 succinic acid Nutrition 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 229920001059 synthetic polymer Polymers 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- RYCLIXPGLDDLTM-UHFFFAOYSA-J tetrapotassium;phosphonato phosphate Chemical compound [K+].[K+].[K+].[K+].[O-]P([O-])(=O)OP([O-])([O-])=O RYCLIXPGLDDLTM-UHFFFAOYSA-J 0.000 description 1
- 239000001577 tetrasodium phosphonato phosphate Substances 0.000 description 1
- 229960000790 thymol Drugs 0.000 description 1
- 230000001131 transforming effect Effects 0.000 description 1
- 229910001428 transition metal ion Inorganic materials 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/20—Halogens; Compounds thereof
- A61K8/21—Fluorides; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/22—Peroxides; Oxygen; Ozone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/24—Phosphorous; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/347—Phenols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
- A61K8/731—Cellulose; Quaternized cellulose derivatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
- A61K8/86—Polyethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
- A61K2800/87—Application Devices; Containers; Packaging
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
- A61K2800/88—Two- or multipart kits
Definitions
- the invention relates to new anti-tartar systems, dentifrice compositions containing these systems and their use in controlling tartar accumulation on teeth.
- Tartar known also as calculus
- calculus is a hard mineralized deposit which forms around teeth. This formation arises from deposition of crystals of calcium phosphate in the pellicle and the extracellular matrix of dental plaque.
- Various forms of calcium phosphate have been identified but the most difficult to remove and thermodynamically most stable form is called hydroxyapatite (HAP).
- HAP hydroxyapatite
- Amorphous forms of calcium phosphate are believed to be the precursors of HAP.
- Regular brushing can usually remove the amorphous forms but is not fully effective to dislodge the final stable calculus form. Therefore it is desirable to prevent amorphous forms of calcium phosphate from transforming into HAP.
- the art has recognized that agents which interfere with the formation of HAP crystallization will be effective anti-tartar agents.
- Soluble inorganic pyrophosphate salts have over the last decade set the commercial standard as tartar control agents. This technology has been reported by Parran, Jr. et al. in a series of patents including U.S. Pat. No. 4,590,077, U.S. Pat. No. 4,515,772 and U.S. Pat. No. 4,684,518.
- Anionic polymers especially carboxylate group functionalized polymers have been widely reported as effective against calculus.
- Commercially most significant has been the use of synthetic, linear anionic polymers of higher molecular weight in combination with the inorganic pyrophosphates.
- This technology derives from work done by Gaffar et al. reported in a series of patents including U.S. Pat. No. 4,627,977, U.S. Pat. No. 4,806,340, U.S. Pat. No. 4,806,342, U.S. Pat. No. 4,808,400 and U.S. Pat. No. 4,808,401.
- Anionic polymers described therein were found to inhibit the action of pyrophosphatase in the mouth and therefore allowing greater efficacy of the inorganic pyrophosphate.
- the commercially operative polymer is a methyl vinyl ether/maleic anhydride copolymer, available under the GAF trademark Gantrez.
- EP 0 341 662 (Amjad) cites a tartar inhibiting oral composition that includes a fluoride source, a dental abrasive, a carboxylate polymer and various phosphonic acids and their derivatives.
- a phosphated acrylic acid/hydroxyethyl methacrylate/alkyl methacrylic acid ester copolymer has been suggested in GB 2 139 635B (Causton) as useful in an oral composition for treating teeth.
- a still further object of the present invention is to provide a tartar control product of improved taste, safety and appearance.
- An anti-tartar dental product comprising:
- composition including:
- a first composition comprising from about 0.01 to about 30% by weight of a water-soluble calcium phosphate or monolithic combination of water soluble calcium and phosphate salts, the composition having a pH less than 7;
- a second composition including from about 0.01 to about 30% by weight of an alkaline material and an anti-caries effective amount of a fluoride ion source, the second composition having a pH greater than 7.5 and stored separately from the first composition in a manner to avoid contact between the phosphate and the alkaline material;
- a method for controlling dental tartar which includes:
- a first composition comprising from about 0.01 to about 30% by weight of a water-soluble calcium phosphate or monolithic combination of water soluble calcium and phosphate salts, the composition having a pH less than 7;
- a second composition comprising from about 0.01 to about 30% by weight of an alkaline material and an anti-caries effective amount of a fluoride ion source, the second composition having a pH greater than 7.5 and stored separately from the first composition in a manner to avoid contact between the phosphate and the alkaline material;
- compositions according to the present invention is not limited to unitary albeit multicompartmented dispensers nor to totally segregated compartments.
- the dispenser may be a system in the form of two individual tubes quite separate from one another but packaged within a kit. Ribbons of the dentifrice from each tube are delivered to a toothbrush with mixing of the compositions occurring in the mouth. Delivery may also be from a single chambered tube except that each of the two compositions are semi solid strips positioned side-by-side touching but not mixing with one another. The relatively high viscosity of the products prevents any substantial transference of either pH change or components between the two strips. Illustrative of this technology is a U.S. product sold by Colgate® under the Baking Soda & Peroxide brand.
- Still another method of delivery may be a single composition such as a paste or gel housing an alkaline environment.
- Monocalcium phosphate compositions may be dispersed throughout the alkaline composition yet separated from contact by a coating encapsulating the phosphate. Activation occurs in the mouth through the presence of water or saliva which penetrates the encapsulating coating releasing phosphate salt to interact with the alkaline environment.
- a critical component of the first composition of this invention is a water soluble calcium phosphate salt.
- water soluble is meant a solubility of at least 0.1 gram in 100 ml water at 25° C. Most preferred is monocalcium hydrogen phosphate but also of potential use are calcium polyol phosphates (e.g. calcium glycerophosphate) and monocalcium ammonium phosphate salts.
- Monolithic compositions of water soluble calcium and phosphate salts may be employed as alternatives to pre-formed water soluble calcium phosphates.
- monolithic is meant separate water soluble calcium salts and phosphate salts which from solution may metathesize into calcium phosphates in solution or later upon mixing with the second composition.
- Illustrative calcium salts include the halides, sulphates, nitrates, citrates, sugars and C 1 -C 6 carboxylates. Most preferred is calcium chloride, calcium sulphate and calcium acetate.
- the monolithic partner phosphate salts may be alkali, ammonium or combination salts thereof. Examples include sodium ammonium phosphate, sodium phosphate, ammonium phosphate and potassium phosphate.
- the water-soluble calcium phosphate salts or the monolithic calcium and phosphate salts (by weight of calcium and phosphate ions only) may be present in amounts ranging from 0.01 to 30%, preferably from 0.1 to 20%, optimally from 1 to 10% by weight of the first composition.
- Solubility of the phosphate salt is maintained in the first composition by having an acidic environment.
- the pH will be less than 7, preferably from 1 to 6.5, more preferably from 1.8 to 6, optimally from 2.5 to 5.5.
- the second composition of the present invention requires an alkaline material so that the second composition has a pH greater than 7, preferably from 7.2 to 11, more preferably from 8 to 10, optimally from 8.5 to 9.5.
- Alkaline materials suitable to achieve the pH are sodium bicarbonate, potassium bicarbonate, sodium carbonate, potassium carbonate, calcium carbonate, calcium oxide, sodium hydroxide, potassium hydroxide and mixtures thereof.
- Amounts of the alkaline material may range from 0.1 to 60%, preferably from 0.5 to 30%, more preferably from 1 to 20%, optimally from 3 to 15% by weight of the second composition.
- compositions of this invention may contain a fluoride anti-caries compound.
- fluoride anti-caries compound examples include sodium fluoride, potassium fluoride, calcium fluoride, magnesium fluoride, stannous fluoride, stannous monofluorophosphate, sodium monofluorophosphate and copper fluoride. Most preferred is sodium fluoride. These sources should release anywhere from about 25 to about 5,000 ppm of fluoride ion.
- the anti-caries compound will normally be present in an amount from about 0.01 to about 5%, preferably from 0.1 to 2.5%, optimally from 0.2 to 1.5% by weight of combined first and second compositions.
- compositions of the present invention may be in the form of either a toothpaste, gel, powder or mouthwash. Most preferably the compositions are either pastes or gels. Especially suitable is where the phosphate salt is incorporated in a gel and the alkaline material incorporated into a paste. These compositions may include water or be anhydrous.
- the phosphate salt as well as the alkaline material will be delivered through a pharmaceutically acceptable carrier.
- pharmaceutically acceptable carrier will include such functional ingredients as water, humectants, abrasives, thickeners, surfactants and combinations thereof. Total levels of these materials may range anywhere from about 1 to about 99%, preferably from 20 to 80%, optimally from 30 to 60% by weight.
- Acidity in the first composition may be achieved by formulating with a peroxide such as hydrogen peroxide, inorganic acids such as phosphoric, hydrochloric, nitric or boric acids, and organic C 2 -C 20 carboxylic acids such as citric, malic, lactic, alginic, succinic, tartaric and ascorbic acids.
- Soluble salts may also be employed such as potassium bitartrate, sodium acid citrate, acid phosphate and pyrophosphate salts such as monosodium phosphate and disodium pyrophosphate.
- Levels of the acidity inducing substances may range in amounts from about 0.1 to about 20%, preferably from about 0.5 to about 10%, optimally from 1.0 to 8% by weight of the first composition. Hydrogen peroxide and phosphoric acid are the preferred substances.
- water when present may range in amounts from about 1 to 95%, preferably from 20 to 60%, optimally from 30 to 50% by weight of each of the compositions.
- some formulations may be anhydrous.
- Humectants are usually also present as one of the carriers. Illustrative of this category are sorbitol, maltitol, mannitol, glycerin and polyethylene glycols (e.g. Carbowax). Amounts of the humectant may range from 1 to 60%, preferably from about 5 to about 50%, optimally from 10 to 40% by weight of each composition.
- Abrasives are normally present in toothpastes and some gels. These may include sodium metaphosphate, dicalcium phosphate (which is not considered a water-soluble phosphate), calcium pyrophosphate, silica, alumina, chalk, insoluble bicarbonate salts, and mixtures thereof. Amounts of the abrasives may range from about 1 to about 80%, preferably from 5 to 50% by weight of each composition.
- Thickeners are a further type of carrier which can be included in the compositions of this invention.
- Illustrative thickeners such as sodium carboxy-methyl cellulose, hydroxy ethyl cellulose, methyl cellulose, ethyl cellulose, gum tragacanth, gum arabic, gum karaya, sodium alginate, carrageenan, guar, xanthan gum, Irish moss, starch, modified starch, Carbomers (crosslinked acrylates) and mixtures thereof.
- Inorganic substances may also be suitable, especially silica aerogels and magnesium aluminum silicate (e.g. Veegum).
- Amounts of the thickener may range from about 0.01 to about 30%, preferably from 0.1 to 20%, optimally from 0.5 to 15% by weight of a composition.
- Surfactants are also considered to be within the carrier definition.
- Surfactants may either be anionic, nonionic, cationic or amphoteric. Most preferred are sodium lauryl sulphate, sodium dodecylbenzene sulphonate and sodium lauryl sarcosinate.
- Surfactants may be present in an amount from about 0.5 to about 10%, preferably from 0.8 to 5% by weight of a composition.
- Gel compositions are structured with substances than can be characterized as either humectants or surfactants.
- a typical gel structurant is a polyoxyethylene-polyoxypropylene copolymer such as those sold by the BASF Corporation under the trademark Pluronic® F88, F99, F108 and F127. These materials are also known as Poloxamers and employed in amounts from about 5 to about 30%, preferably between about 18 and about 25% by weight of a composition.
- Flavors may also be present in the compositions. These flavors may be based on oils of spearmint and peppermint. Examples of other flavoring materials include menthol, clove, wintergreen, eucalyptus and aniseed. Flavors may range in concentration from about 0.1 to about 5% by weight of a composition.
- Sweetening agents may also be included such as saccharin, sodium cyclamate, aspartame, ace-sulfame, xylitol and combinations thereof at levels from 0.1 to 10% by weight of a composition.
- Gel compositions incorporating hydrogen peroxide may include a sequestering agent(s) such as a pyrophosphate or other phosphate for chelation of ferric/ferrous ion as well as other transition metal ions to enhance hydrogen peroxide stability.
- the sequestering agents may also be included within the paste compositions and are present in amounts from about 0.01 to about 20% by weight of a composition.
- Most preferred chelatants are tetrasodium pyrophosphate, sodium tripolyphosphate and sodium hexametaphosphate, all known to be effective at lower pH with little affinity for calcium ion.
- Other organic chelating agents such as sodium citrate and zinc citrate are also useful.
- additives may also be incorporated such as preservatives, silicones, other synthetic or natural polymers such as Gantrez S97®, additional anti-tartar actives and antigingivitis actives.
- additional anti-tartar agents are included zinc citrate, tetrasodium pyrophosphate, disodium pyrophosphate, dipotassium pyrophosphate, tetrapotassium pyrophosphate and mixtures thereof.
- Antigingivitis actives may include thymol, Triclosan, stannous gluconate and mixtures thereof. Amounts of each of the aforementioned ingredients will depend upon their function. Generally each of these substances will range in amounts from about 0.01 to about 20% by weight of a composition.
- Typical of the present invention is a first composition in the form of a gel and a second composition in the form of a paste.
- Each of these formulations is held in a separate compartment of a dual-compartment dispenser similar to that disclosed in U.S. Pat. No. 5,038,963 (Pettengill et al.).
- Another system typical of the present invention is a two part toothpaste. Each part is placed in a dual-compartment dispenser similar to that of Example 1.
- PASTE 2A PASTE 2B COMPONENTS (% WEIGHT) (% WEIGHT) Sorbitol 70% Active 28.50 — Syloid 63XX (Hydrated Silica) 20.00 18.0 Glycerin 28.00 32.0 Monocalcium Phosphate 6.49 — Citric Acid 5.00 — Syloid 244 (Thickening Silica) 3.00 0.5 Xanthan Gum 0.50 — Sodium Fluoride — 0.44 FD&C Blue No. 1 0.01 — Sodium Bicarbonate — 25.0 Sodium Lauryl Sulphate — 1.5 Sodium Carboxymethyl Cellulose — 0.8 Flavor — 1.0 Titanium Dioxide — 0.4 Sodium Saccharin — 0.2 Water balance balance balance
- Paste 2A The pH of Paste 2A is approximately 2.0.
- Paste 2B has a pH of approximately 9.0. Strips of each of these are extruded onto a toothbrush. These strips are then brushed against the teeth thereby mixing them together.
- Yet another system typical of the present invention is a two part toothpaste as described below. Each part is placed in a dual-compartment dispenser similar to that of Example 1.
- PASTE 3A PASTE 3B COMPONENTS (% WEIGHT) (% WEIGHT) Sorbitol (70% Active) 30.50 — Alumina 20.00 18.0 Polyol II 10.00 32.0 Malic Acid 5.00 — Monocalcium Phosphate 4.50 — Syloid 244 (Thickening Silica) 3.00 0.5 Xanthan Gum 0.50 — Sodium Fluoride — 0.44 FD&C Blue No. 1 0.01 — Sodium Bicarbonate — 25.0 Sodium Lauryl Sulphate — 1.5 Sodium Carboxymethyl Cellulose — 0.8 Flavor — 1.0 Sodium Carbonate — 0.4 Sodium Saccharin — 0.2 Water balance balance balance balance
- Paste 3A and 3B respectively are approximately 2 and 9. Strips of each of these pastes are placed onto a toothbrush. These strips are then brushed against the teeth thereby mixing them together.
- This Example illustrates use of a monolithic calcium and phosphate salt combination to deliver the water soluble monocalcium phosphate component.
- Separate gel and paste formulations representing the first and second compositions of this invention were prepared with the following compositions.
- Yet another system typical of the present invention is a two part toothpaste as described below. Each part is placed in a dual compartment dispenser similar to that of Example 1.
- This Example illustrates use of monocalcium phosphate in a Gel composition along with Triclosan solubilized in alcohol.
- Triclosan is incorporated into a Paste composition of elevated pH for eventual combination with the Gel.
- Example 1 A clinical trial was conducted to compare the dental product of Example 1 with an identical product that did not include monocalcium phosphate monohydrate.
- the commercial toothpastes Aim® and Colgate Total® were used as reference samples, the latter product being a formulation containing triclosan.
- Protocol for the clinical was as follows. Panelists were carefully selected to meet a long list of criteria such as exhibiting visible tartar within only 1 to 2 months of a professional cleaning. Tartar present on the lingual aspect of the 6 anterior Mandibular teeth was evaluated according to the Volpe/Manhold Scoring Index. Following an initial tartar assessment, each panelist received a thorough dental cleaning. Panelists were then given Aim® toothpaste for use over the following 3 weeks to allow tartar to build. Another tartar evaluation identified the baseline for a panelist's normal tartar growth rate. A second dental prophylaxis was then performed to remove dental tartar rendering the panelists ready to receive the first test product (Example 1 with monocalcium phosphate monohydrate). Tartar evaluations were then conducted after 2 and 3 weeks of product usage. Aim® was then given to the panelists for a 4 week washout period.
- the Mandibular Anterior teeth were then scaled to remove tartar buildup over the washout period. Panelists were next assigned to use Colgate Total® for the subsequent 3 weeks. Evaluations were again conducted after the 2 and 3 week usage period. In a further phase of the test, the panelists were directed to use Aim® for another 4 week washout. Again, the Mandibular Anterior teeth were scaled to remove tartar buildup over the 4 week washout period. Panelists were then assigned to Example 1 where monocalcium phosphate monohydrate was absent (replaced by 2% zinc citrate) for the next 3 weeks. Tartar evaluations were conducted at the 2 and 3 week interval. Results of the tests are reported in the Table below.
- Example 1 containing calcium phosphate had significantly better calculus inhibition performance than Aim®. The better performance is attributed to calcium phosphate which when absent from Example 1 allowed considerable more calculus formation.
- Paste Composition 9A INGREDIENT WEIGHT % Polyol II (70% Sorbitol) 33.30 Syloid 63XX (Hydrated Silica) 30.00 Sodium Bicarbonate 10.00 Sylox 15X 2.00 Polyethylene Glycol 1450 (PEG 32) 5.00 Sodium Lauryl Sulphate 2.98 Alcohol 38B 2.84 Flavor 1.30 Cellulose Gum 0.80 Saccharin 0.54 Menthol 0.50 Sodium Fluoride 0.44 Titanium Dioxide 0.30 Water Balance
- the gel compositions (containing monocalcium phosphate monohydrate) were different for each of the test cells.
- the formulations are reported in the Tables below.
- Table II provides the calculus reduction % results.
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Abstract
An oral product and method is provided for inhibiting tartar formation on the teeth. The product is housed in a container and includes a first composition containing a water soluble calcium phosphate salt or monolithic combination of calcium and phosphate salts in a carrier with the first composition having a pH less than 7, and a second composition containing an alkaline material and a fluoride ion source in a carrier to achieve a pH greater than 7.5. The first and second compositions are separated from one another prior to use. When combined upon application to the teeth, the first and second compositions form a system for inhibiting tartar around the teeth.
Description
This is a Divisional application of Ser. No. 09/395,064 filed Sep. 13, 1999, which arises from U.S. Provisional Application Serial No. 60/129,779 filed Apr. 16, 1999.
1. Field of the Invention
The invention relates to new anti-tartar systems, dentifrice compositions containing these systems and their use in controlling tartar accumulation on teeth.
2. The Related Art
Tartar, known also as calculus, is a hard mineralized deposit which forms around teeth. This formation arises from deposition of crystals of calcium phosphate in the pellicle and the extracellular matrix of dental plaque. Various forms of calcium phosphate have been identified but the most difficult to remove and thermodynamically most stable form is called hydroxyapatite (HAP). Amorphous forms of calcium phosphate are believed to be the precursors of HAP. Regular brushing can usually remove the amorphous forms but is not fully effective to dislodge the final stable calculus form. Therefore it is desirable to prevent amorphous forms of calcium phosphate from transforming into HAP. The art has recognized that agents which interfere with the formation of HAP crystallization will be effective anti-tartar agents.
Soluble inorganic pyrophosphate salts have over the last decade set the commercial standard as tartar control agents. This technology has been reported by Parran, Jr. et al. in a series of patents including U.S. Pat. No. 4,590,077, U.S. Pat. No. 4,515,772 and U.S. Pat. No. 4,684,518.
Anionic polymers, especially carboxylate group functionalized polymers have been widely reported as effective against calculus. Commercially most significant has been the use of synthetic, linear anionic polymers of higher molecular weight in combination with the inorganic pyrophosphates. This technology derives from work done by Gaffar et al. reported in a series of patents including U.S. Pat. No. 4,627,977, U.S. Pat. No. 4,806,340, U.S. Pat. No. 4,806,342, U.S. Pat. No. 4,808,400 and U.S. Pat. No. 4,808,401. Anionic polymers described therein were found to inhibit the action of pyrophosphatase in the mouth and therefore allowing greater efficacy of the inorganic pyrophosphate. The commercially operative polymer is a methyl vinyl ether/maleic anhydride copolymer, available under the GAF trademark Gantrez.
Organic phosphonic acid derivatives, some in polymeric form, have been disclosed in U.S. Pat. No. 3,934,002 (Haefele). EP 0 341 662 (Amjad) cites a tartar inhibiting oral composition that includes a fluoride source, a dental abrasive, a carboxylate polymer and various phosphonic acids and their derivatives. A phosphated acrylic acid/hydroxyethyl methacrylate/alkyl methacrylic acid ester copolymer has been suggested in GB 2 139 635B (Causton) as useful in an oral composition for treating teeth.
Evident from the foregoing review of the art is the considerable effort expended to devise better tartar control compositions. By no means, however, has any of the reported art been able to more than attenuate the problem. There is considerable room for improvement over the known control agents.
Accordingly, it is an object of the present invention to provide a product of improved efficacy in controlling formation of tartar.
A still further object of the present invention is to provide a tartar control product of improved taste, safety and appearance.
These and other objects of the present invention will become more apparent in light of the detailed description and Examples which follow.
An anti-tartar dental product is provided comprising:
(i) a container;
(ii) an oral composition stored within the container, the composition including:
(a) a first composition comprising from about 0.01 to about 30% by weight of a water-soluble calcium phosphate or monolithic combination of water soluble calcium and phosphate salts, the composition having a pH less than 7; and
(b) a second composition including from about 0.01 to about 30% by weight of an alkaline material and an anti-caries effective amount of a fluoride ion source, the second composition having a pH greater than 7.5 and stored separately from the first composition in a manner to avoid contact between the phosphate and the alkaline material;
(iii) instructions printed on the container directing use of the composition to control tartar when applied to the teeth.
A method is provided for controlling dental tartar which includes:
(i) obtaining a product which includes:
(a) a first composition comprising from about 0.01 to about 30% by weight of a water-soluble calcium phosphate or monolithic combination of water soluble calcium and phosphate salts, the composition having a pH less than 7; and
(b) a second composition comprising from about 0.01 to about 30% by weight of an alkaline material and an anti-caries effective amount of a fluoride ion source, the second composition having a pH greater than 7.5 and stored separately from the first composition in a manner to avoid contact between the phosphate and the alkaline material;
(ii) extruding a portion of first and second compositions onto a toothbrush; and
(iii) brushing the teeth with the combination of first and second compositions.
Products intended for remineralization of teeth ordinarily employ calcium and phosphate ions. Naturally there is great concern that these ions can be diverted from remineralization to calculus forming hydroxyapatite. Now it has been discovered that when a water soluble calcium phosphate salt is stored within one composition held at a low pH and mixed after storage with a second composition having a high pH, the result is a significant reduction in normal tartar formation against the teeth.
Separate storage of the two compositions of this invention may be accomplished through a dual compartment dispenser. U.S. Pat. No. 4,687,663 (Schaeffer) discloses a dual-compartment package respectively storing a peroxide gel and a bicarbonate paste. Pump packaging with multiple compartments is reported in U.S. Pat. No. 5,038,963 (Pettengill et al.) and U.S. Pat. No. 5,020,694 (Pettengill) which are embodied in a U.S. product known as Mentadent® Baking Soda & Peroxide toothpaste.
Of course, delivery of compositions according to the present invention is not limited to unitary albeit multicompartmented dispensers nor to totally segregated compartments. The dispenser may be a system in the form of two individual tubes quite separate from one another but packaged within a kit. Ribbons of the dentifrice from each tube are delivered to a toothbrush with mixing of the compositions occurring in the mouth. Delivery may also be from a single chambered tube except that each of the two compositions are semi solid strips positioned side-by-side touching but not mixing with one another. The relatively high viscosity of the products prevents any substantial transference of either pH change or components between the two strips. Illustrative of this technology is a U.S. product sold by Colgate® under the Baking Soda & Peroxide brand. Still another method of delivery may be a single composition such as a paste or gel housing an alkaline environment. Monocalcium phosphate compositions may be dispersed throughout the alkaline composition yet separated from contact by a coating encapsulating the phosphate. Activation occurs in the mouth through the presence of water or saliva which penetrates the encapsulating coating releasing phosphate salt to interact with the alkaline environment.
A critical component of the first composition of this invention is a water soluble calcium phosphate salt. By the term “water soluble” is meant a solubility of at least 0.1 gram in 100 ml water at 25° C. Most preferred is monocalcium hydrogen phosphate but also of potential use are calcium polyol phosphates (e.g. calcium glycerophosphate) and monocalcium ammonium phosphate salts. Monolithic compositions of water soluble calcium and phosphate salts may be employed as alternatives to pre-formed water soluble calcium phosphates. By the term “monolithic” is meant separate water soluble calcium salts and phosphate salts which from solution may metathesize into calcium phosphates in solution or later upon mixing with the second composition. Illustrative calcium salts include the halides, sulphates, nitrates, citrates, sugars and C1-C6 carboxylates. Most preferred is calcium chloride, calcium sulphate and calcium acetate. The monolithic partner phosphate salts may be alkali, ammonium or combination salts thereof. Examples include sodium ammonium phosphate, sodium phosphate, ammonium phosphate and potassium phosphate. The water-soluble calcium phosphate salts or the monolithic calcium and phosphate salts (by weight of calcium and phosphate ions only) may be present in amounts ranging from 0.01 to 30%, preferably from 0.1 to 20%, optimally from 1 to 10% by weight of the first composition.
Solubility of the phosphate salt is maintained in the first composition by having an acidic environment. The pH will be less than 7, preferably from 1 to 6.5, more preferably from 1.8 to 6, optimally from 2.5 to 5.5.
The second composition of the present invention requires an alkaline material so that the second composition has a pH greater than 7, preferably from 7.2 to 11, more preferably from 8 to 10, optimally from 8.5 to 9.5. Alkaline materials suitable to achieve the pH are sodium bicarbonate, potassium bicarbonate, sodium carbonate, potassium carbonate, calcium carbonate, calcium oxide, sodium hydroxide, potassium hydroxide and mixtures thereof. Amounts of the alkaline material may range from 0.1 to 60%, preferably from 0.5 to 30%, more preferably from 1 to 20%, optimally from 3 to 15% by weight of the second composition.
Advantageously, compositions of this invention, especially the second composition may contain a fluoride anti-caries compound. Illustrative of such fluoride compounds are sodium fluoride, potassium fluoride, calcium fluoride, magnesium fluoride, stannous fluoride, stannous monofluorophosphate, sodium monofluorophosphate and copper fluoride. Most preferred is sodium fluoride. These sources should release anywhere from about 25 to about 5,000 ppm of fluoride ion. The anti-caries compound will normally be present in an amount from about 0.01 to about 5%, preferably from 0.1 to 2.5%, optimally from 0.2 to 1.5% by weight of combined first and second compositions.
The compositions of the present invention may be in the form of either a toothpaste, gel, powder or mouthwash. Most preferably the compositions are either pastes or gels. Especially suitable is where the phosphate salt is incorporated in a gel and the alkaline material incorporated into a paste. These compositions may include water or be anhydrous.
The phosphate salt as well as the alkaline material will be delivered through a pharmaceutically acceptable carrier. The term “pharmaceutically acceptable carrier” will include such functional ingredients as water, humectants, abrasives, thickeners, surfactants and combinations thereof. Total levels of these materials may range anywhere from about 1 to about 99%, preferably from 20 to 80%, optimally from 30 to 60% by weight.
Acidity in the first composition may be achieved by formulating with a peroxide such as hydrogen peroxide, inorganic acids such as phosphoric, hydrochloric, nitric or boric acids, and organic C2-C20 carboxylic acids such as citric, malic, lactic, alginic, succinic, tartaric and ascorbic acids. Soluble salts may also be employed such as potassium bitartrate, sodium acid citrate, acid phosphate and pyrophosphate salts such as monosodium phosphate and disodium pyrophosphate. Levels of the acidity inducing substances may range in amounts from about 0.1 to about 20%, preferably from about 0.5 to about 10%, optimally from 1.0 to 8% by weight of the first composition. Hydrogen peroxide and phosphoric acid are the preferred substances.
Among the carriers, water when present may range in amounts from about 1 to 95%, preferably from 20 to 60%, optimally from 30 to 50% by weight of each of the compositions. Of course some formulations may be anhydrous.
Humectants are usually also present as one of the carriers. Illustrative of this category are sorbitol, maltitol, mannitol, glycerin and polyethylene glycols (e.g. Carbowax). Amounts of the humectant may range from 1 to 60%, preferably from about 5 to about 50%, optimally from 10 to 40% by weight of each composition.
Abrasives are normally present in toothpastes and some gels. These may include sodium metaphosphate, dicalcium phosphate (which is not considered a water-soluble phosphate), calcium pyrophosphate, silica, alumina, chalk, insoluble bicarbonate salts, and mixtures thereof. Amounts of the abrasives may range from about 1 to about 80%, preferably from 5 to 50% by weight of each composition.
Thickeners are a further type of carrier which can be included in the compositions of this invention. Illustrative thickeners such as sodium carboxy-methyl cellulose, hydroxy ethyl cellulose, methyl cellulose, ethyl cellulose, gum tragacanth, gum arabic, gum karaya, sodium alginate, carrageenan, guar, xanthan gum, Irish moss, starch, modified starch, Carbomers (crosslinked acrylates) and mixtures thereof. Inorganic substances may also be suitable, especially silica aerogels and magnesium aluminum silicate (e.g. Veegum). Amounts of the thickener may range from about 0.01 to about 30%, preferably from 0.1 to 20%, optimally from 0.5 to 15% by weight of a composition.
Surfactants are also considered to be within the carrier definition. Surfactants may either be anionic, nonionic, cationic or amphoteric. Most preferred are sodium lauryl sulphate, sodium dodecylbenzene sulphonate and sodium lauryl sarcosinate. Surfactants may be present in an amount from about 0.5 to about 10%, preferably from 0.8 to 5% by weight of a composition.
Gel compositions are structured with substances than can be characterized as either humectants or surfactants. For instance, a typical gel structurant is a polyoxyethylene-polyoxypropylene copolymer such as those sold by the BASF Corporation under the trademark Pluronic® F88, F99, F108 and F127. These materials are also known as Poloxamers and employed in amounts from about 5 to about 30%, preferably between about 18 and about 25% by weight of a composition.
Flavors may also be present in the compositions. These flavors may be based on oils of spearmint and peppermint. Examples of other flavoring materials include menthol, clove, wintergreen, eucalyptus and aniseed. Flavors may range in concentration from about 0.1 to about 5% by weight of a composition.
Sweetening agents may also be included such as saccharin, sodium cyclamate, aspartame, ace-sulfame, xylitol and combinations thereof at levels from 0.1 to 10% by weight of a composition.
Gel compositions incorporating hydrogen peroxide may include a sequestering agent(s) such as a pyrophosphate or other phosphate for chelation of ferric/ferrous ion as well as other transition metal ions to enhance hydrogen peroxide stability. The sequestering agents may also be included within the paste compositions and are present in amounts from about 0.01 to about 20% by weight of a composition. Most preferred chelatants are tetrasodium pyrophosphate, sodium tripolyphosphate and sodium hexametaphosphate, all known to be effective at lower pH with little affinity for calcium ion. Other organic chelating agents such as sodium citrate and zinc citrate are also useful.
Other additives may also be incorporated such as preservatives, silicones, other synthetic or natural polymers such as Gantrez S97®, additional anti-tartar actives and antigingivitis actives. Among the additional anti-tartar agents are included zinc citrate, tetrasodium pyrophosphate, disodium pyrophosphate, dipotassium pyrophosphate, tetrapotassium pyrophosphate and mixtures thereof. Antigingivitis actives may include thymol, Triclosan, stannous gluconate and mixtures thereof. Amounts of each of the aforementioned ingredients will depend upon their function. Generally each of these substances will range in amounts from about 0.01 to about 20% by weight of a composition.
Except in the operating and comparative examples, or where otherwise explicitly indicated, all numbers in this description indicating amounts of material ought to be understood as modified by the word “about”.
The following examples will more fully illustrate the embodiments of this invention. All parts, percentages and proportions referred to herein and in the appended claims are by weight of either the first or second composition unless otherwise indicated.
Typical of the present invention is a first composition in the form of a gel and a second composition in the form of a paste. Each of these formulations is held in a separate compartment of a dual-compartment dispenser similar to that disclosed in U.S. Pat. No. 5,038,963 (Pettengill et al.).
INGREDIENT | WEIGHT % | ||
Gel Composition 1A |
Glycerin | 40.00 | |
Pluronic F-127 | 20.00 | |
Monocalcium Phosphate Monohydrate | 1.60 | |
Hydrogen Peroxide (35% Active) | 4.285 | |
Phosphoric Acid | 0.40 | |
FD&C Blue No. 1 | 0.01 | |
Water | Balance |
Paste Composition 1B |
Polyol II (70% Sorbitol) | 47.00 | ||
Syloid 63XX (Hydrated Silica) | 15.00 | ||
Sodium Bicarbonate | 10.00 | ||
Sylox 15X | 6.00 | ||
Polyethylene Glycol 1450 (PEG-32) | 5.00 | ||
Ethyl Alcohol 38B | 2.84 | ||
Sodium Lauryl Sulphate | 2.98 | ||
Flavor | 1.10 | ||
Cellulose Gum | 0.80 | ||
Sodium Saccharin | 0.54 | ||
Menthol | 0.50 | ||
Sodium Fluoride | 0.44 | ||
Titanium Dioxide | 0.30 | ||
Water | Balance | ||
Another system typical of the present invention is a two part toothpaste. Each part is placed in a dual-compartment dispenser similar to that of Example 1.
PASTE 2A | PASTE 2B | |
COMPONENTS | (% WEIGHT) | (% WEIGHT) |
Sorbitol 70% Active | 28.50 | — |
Syloid 63XX (Hydrated Silica) | 20.00 | 18.0 |
Glycerin | 28.00 | 32.0 |
Monocalcium Phosphate | 6.49 | — |
Citric Acid | 5.00 | — |
Syloid 244 (Thickening Silica) | 3.00 | 0.5 |
Xanthan Gum | 0.50 | — |
Sodium Fluoride | — | 0.44 |
FD&C Blue No. 1 | 0.01 | — |
Sodium Bicarbonate | — | 25.0 |
Sodium Lauryl Sulphate | — | 1.5 |
Sodium Carboxymethyl Cellulose | — | 0.8 |
Flavor | — | 1.0 |
Titanium Dioxide | — | 0.4 |
Sodium Saccharin | — | 0.2 |
Water | balance | balance |
The pH of Paste 2A is approximately 2.0. Paste 2B has a pH of approximately 9.0. Strips of each of these are extruded onto a toothbrush. These strips are then brushed against the teeth thereby mixing them together.
Yet another system typical of the present invention is a two part toothpaste as described below. Each part is placed in a dual-compartment dispenser similar to that of Example 1.
PASTE 3A | PASTE 3B | |
COMPONENTS | (% WEIGHT) | (% WEIGHT) |
Sorbitol (70% Active) | 30.50 | — |
Alumina | 20.00 | 18.0 |
Polyol II | 10.00 | 32.0 |
Malic Acid | 5.00 | — |
Monocalcium Phosphate | 4.50 | — |
Syloid 244 (Thickening Silica) | 3.00 | 0.5 |
Xanthan Gum | 0.50 | — |
Sodium Fluoride | — | 0.44 |
FD&C Blue No. 1 | 0.01 | — |
Sodium Bicarbonate | — | 25.0 |
Sodium Lauryl Sulphate | — | 1.5 |
Sodium Carboxymethyl Cellulose | — | 0.8 |
Flavor | — | 1.0 |
Sodium Carbonate | — | 0.4 |
Sodium Saccharin | — | 0.2 |
Water | balance | balance |
The pH of Paste 3A and 3B respectively are approximately 2 and 9. Strips of each of these pastes are placed onto a toothbrush. These strips are then brushed against the teeth thereby mixing them together.
This Example illustrates use of a monolithic calcium and phosphate salt combination to deliver the water soluble monocalcium phosphate component. Separate gel and paste formulations representing the first and second compositions of this invention were prepared with the following compositions.
INGREDIENT | WEIGHT % |
Gel Composition 4A |
Glycerin | 40.00 | |
Pluronic F-127 ® | 20.00 | |
Hydrogen Peroxide (35% Active) | 4.29 | |
Calcium Chloride Dihydrate | 2.10 | |
Dibasic Sodium Phosphate | 1.00 | |
Phosphoric Acid (85% Active) | 1.50 | |
Sodium Citrate | 0.53 | |
FD&C Blue No. 1 | 0.01 | |
Water | Balance |
Paste Composition 4B |
Polyol II (70% Sorbitol) | 40.50 | ||
Syloid 63XX (Hydrated Silica) | 15.00 | ||
Sodium Bicarbonate | 10.00 | ||
Sylox 15X | 6.00 | ||
Polyethylene Glycol 1450 (PEG-32) | 3.00 | ||
Ethyl Alcohol 38B | 2.84 | ||
Sodium Lauryl Sulphate | 2.98 | ||
Flavor | 1.10 | ||
Cellulose Gum | 0.80 | ||
Sodium Saccharin | 0.54 | ||
Menthol | 0.50 | ||
Sodium Fluoride | 0.44 | ||
Titanium Dioxide | 0.30 | ||
Water | Balance | ||
Yet another system typical of the present invention is a two part toothpaste as described below. Each part is placed in a dual compartment dispenser similar to that of Example 1.
INGREDIENT | WEIGHT % | ||
Gel Composition 5A |
Glycerin | 40.00 | |
Pluronic F-127 | 20.00 | |
Monocalcium Phosphate Monohydrate | 3.10 | |
Phosphoric Acid (85% Active) | 0.85 | |
Water | Balance |
Paste Composition 5B |
Polyol II (70% Sorbitol) | 46.68 | ||
Syloid 63XX (Hydrated Silica) | 15.00 | ||
Sodium Carbonate | 6.50 | ||
Sylox 15X (Hydrated Silica) | 6.00 | ||
Polyethylene Glycol 1450 (PEG 32) | 5.00 | ||
Ethyl Alcohol 38B | 2.84 | ||
Sodium Lauryl Sulphate | 2.98 | ||
Flavor | 1.00 | ||
Cellulose Gum | 0.80 | ||
Sodium Saccharin | 0.50 | ||
Menthol | 0.50 | ||
Sodium fluoride | 0.44 | ||
Titanium Dioxide | 0.30 | ||
Water | Balance | ||
The pH of 5A and 5B respectively are approximately 2.7 and 9.5 |
This Example illustrates use of monocalcium phosphate in a Gel composition along with Triclosan solubilized in alcohol.
INGREDIENT | WEIGHT % | ||
Gel Composition 6A |
Glycerin | 40.00 | |
Pluronic F-127 | 20.00 | |
Alcohol SDA 38B | 5.00 | |
Monocalcium Phosphate, Monohydrate | 1.55 | |
Phosphoric Acid (95% Active) | 0.45 | |
Hydrogen Peroxide (35% Active) | 4.29 | |
Irgacare ® MP (Triclosan) | 0.67 | |
Water | Balance |
Paste Composition 6B |
Polyol II 70% Sorbitol | 46.68 | ||
Syloid 63XX (Hydrated Silica) | 15.00 | ||
Sodium Bicarbonate | 10.00 | ||
Sylox 15X (Hydrated Silica) | 6.00 | ||
Polyethylene Glycol 1450 (PEG 32) | 3.00 | ||
Ethyl Alcohol 38B | 2.84 | ||
Sodium Lauryl Sulphate | 2.98 | ||
Flavor | 1.10 | ||
Cellulose Gum | 0.80 | ||
Sodium Saccharin | 0.54 | ||
Menthol | 0.50 | ||
Sodium Fluoride | 0.44 | ||
Titanium Dioxide | 0.30 | ||
Water | Balance | ||
The pH of 6A and 6B respectively are approximately 2.7 and 9.2 |
Another Example is shown using monocalcium phosphate in a Gel composition. Here Triclosan is incorporated into a Paste composition of elevated pH for eventual combination with the Gel.
INGREDIENT | WEIGHT % | ||
Gel Composition 7A |
Glycerin | 40.00 |
Pluronic F-127 | 20.00 |
Hydrogen Peroxide (35% Active) | 4.29 |
Monocalcium Phosphate, Monohydrate | 3.10 |
Phosphoric Acid (95% Active) | 0.85 |
Water | Balance |
Paste Composition 7B |
Polyol II | 44.93 |
Syloid 63XX (Hydrated Silica) | 30.00 |
Sodium Carbonate | 7.00 |
Sylox 15X (hydrated Silica) | 2.00 |
Ethyl Alcohol 38B | 2.84 |
Sodium Lauryl Sulphate | 2.98 |
Flavor | 1.30 |
Irgacare ® MP (Triclosan) | 0.55 |
Sodium Saccharin | 0.54 |
Cellulose Gum | 0.80 |
Menthol | 0.50 |
Sodium fluoride | 0.44 |
Titanium Dioxide | 0.30 |
Water | Balance |
The pH 7A and 7B respectively are approximately 2.7 and 9.2 |
A clinical trial was conducted to compare the dental product of Example 1 with an identical product that did not include monocalcium phosphate monohydrate. The commercial toothpastes Aim® and Colgate Total® were used as reference samples, the latter product being a formulation containing triclosan.
Protocol for the clinical was as follows. Panelists were carefully selected to meet a long list of criteria such as exhibiting visible tartar within only 1 to 2 months of a professional cleaning. Tartar present on the lingual aspect of the 6 anterior Mandibular teeth was evaluated according to the Volpe/Manhold Scoring Index. Following an initial tartar assessment, each panelist received a thorough dental cleaning. Panelists were then given Aim® toothpaste for use over the following 3 weeks to allow tartar to build. Another tartar evaluation identified the baseline for a panelist's normal tartar growth rate. A second dental prophylaxis was then performed to remove dental tartar rendering the panelists ready to receive the first test product (Example 1 with monocalcium phosphate monohydrate). Tartar evaluations were then conducted after 2 and 3 weeks of product usage. Aim® was then given to the panelists for a 4 week washout period.
The Mandibular Anterior teeth were then scaled to remove tartar buildup over the washout period. Panelists were next assigned to use Colgate Total® for the subsequent 3 weeks. Evaluations were again conducted after the 2 and 3 week usage period. In a further phase of the test, the panelists were directed to use Aim® for another 4 week washout. Again, the Mandibular Anterior teeth were scaled to remove tartar buildup over the 4 week washout period. Panelists were then assigned to Example 1 where monocalcium phosphate monohydrate was absent (replaced by 2% zinc citrate) for the next 3 weeks. Tartar evaluations were conducted at the 2 and 3 week interval. Results of the tests are reported in the Table below.
TABLE I |
CALCULUS CLINICAL |
% CALCULUS REDUCTION | ||
AFTER 6 WEEKS | ||
Aim ® | +5 | ||
Colgate Total ® | −30 | ||
Example 1 (Calcium Phosphate) | −42 | ||
Example 1 (Without Calcium | −24 | ||
Phosphate) | |||
Positive values indicate an increase in calculus. Negative values indicate a reduction. Table I reveals that Example 1 containing calcium phosphate had significantly better calculus inhibition performance than Aim®. The better performance is attributed to calcium phosphate which when absent from Example 1 allowed considerable more calculus formation.
A further study was conducted under a protocol similar to that described in Example 8 and utilizing some of the earlier data. All three cells of the test employed the same paste (sodium bicarbonate) composition as outlined below.
Paste Composition 9A |
INGREDIENT | WEIGHT % | ||
Polyol II (70% Sorbitol) | 33.30 | ||
Syloid 63XX (Hydrated Silica) | 30.00 | ||
Sodium Bicarbonate | 10.00 | ||
Sylox 15X | 2.00 | ||
Polyethylene Glycol 1450 (PEG 32) | 5.00 | ||
Sodium Lauryl Sulphate | 2.98 | ||
Alcohol 38B | 2.84 | ||
Flavor | 1.30 | ||
Cellulose Gum | 0.80 | ||
Saccharin | 0.54 | ||
Menthol | 0.50 | ||
Sodium Fluoride | 0.44 | ||
Titanium Dioxide | 0.30 | ||
Water | Balance | ||
The gel compositions (containing monocalcium phosphate monohydrate) were different for each of the test cells. The formulations are reported in the Tables below.
Gel Composition 9B-9D |
WEIGHT % |
COMPOSITION | 9B | 9C | 9D |
Glycerin | 40.00 | 39.00 | 39.00 |
Pluronic F-127 | 20.00 | 21.00 | 21.00 |
Hydrogen Peroxide (35% Active) | 4.285 | 4.285 | 4.285 |
Monocalcium Phosphate Monohydrate | — | 1.07 | — |
Disodium Phosphate | — | 0.20 | — |
Methyl Salicylate | 0.50 | 0.50 | 0.50 |
Calcium Chloride | — | — | 0.92 |
Phosphoric Acid (95% Active) | 0.15 | 0.70 | 0.25 |
Colorant | 0.005 | 0.01 | 0.01 |
Water | Balance | Balance | Balance |
Table II provides the calculus reduction % results.
TABLE II |
Calculus Reduction Results |
TEST | CALCIUM/PHOSPHATE | % CALCULUS |
FORMULATION | (ppm) | REDUCTION |
9A-B | 0.0/3877 | −24 |
9A-C | 810/8000 | −44 |
9A-D | 1250/1380 | −40 |
The study reveals that calcium is essential for a reduction in calculus. Levels of 810 and 1250 ppm calcium in combination with phosphate were sufficient to provide significant calculus reduction.
The foregoing description and examples illustrate selected embodiments of the present invention. In light thereof variations and modifications will be suggested to one skilled in the art, all of which are within the spirit and purview of this invention.
Claims (19)
1. An anti-tartar dental product comprising:
(i) a container;
(ii) an oral composition stored within the container, the composition comprising:
(a) a first composition comprising from about 0.01 to about 30% by weight of a water-soluble calcium phosphate or monolithic combination of water soluble calcium and phosphate salts, the composition having a pH less than 7; and
(b) a second composition including from about 0.01 to about 30% by weight of an alkaline material and an anti-caries effective amount of a fluoride ion source, the second composition having a pH greater than 7.5 and stored separately from the first composition in a manner to avoid contact between the phosphate and the alkaline material.
2. The product according to claim 1 wherein the water-soluble phosphate salt is monocalcium hydrogen phosphate.
3. The product according to claim 1 wherein the alkaline material is selected from the group consisting of sodium bicarbonate, potassium bicarbonate, sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, calcium carbonate, calcium oxide and mixtures thereof.
4. The product according to claim 1 wherein the pH of the first composition ranges from 2.5 to 5.5.
5. The product according to claim 1 wherein the pH of the second composition ranges from 7.2 to 11.
6. The product according to claim 1 wherein the pH of the first composition results from inclusion of a compound selected from the group consisting of hydrogen peroxide, inorganic acids, C2-C20 carboxylic acids and mixtures thereof.
7. The product according to claim 1 wherein the monolithic combination of water soluble calcium salts are selected from the group consisting of calcium chloride, calcium sulphate and calcium acetate and the respective phosphate salts are selected from the group consisting of sodium phosphate, ammonium phosphate and sodium ammonium phosphate.
8. The product according to claim 1 further comprising from about 0.01 to about 20% by weight of triclosan.
9. The product according to claim 1 further comprising from about 0.01 to about 20% by weight of a zinc salt.
10. The product according to claim 1 further comprising from about 0.01 to about 5% by weight of a fluoride compound.
11. A method for controlling dental tartar comprising
(i) obtaining a product which comprises:
(a) a first composition comprising from about 0.01 to about 30% by weight of a water-soluble calcium phosphate or monolithic combination of water soluble calcium and phosphate salts, the composition having a pH less than 7; and
(b) a second composition comprising from about 0.01 to about 30% by weight of an alkaline material and an anti-caries effective amount of a fluoride ion source, the second composition having a pH greater than 7.5 and stored separately from the first composition in a manner to avoid contact between the phosphate and the alkaline material;
(ii) extruding a portion of first and second compositions onto a toothbrush; and
(iii) brushing the teeth with the combination of first and second compositions.
12. The method according to claim 11 wherein the water-soluble phosphate salt is monocalcium hydrogen phosphate.
13. The method according to claim 11 wherein the alkaline material is selected from the group consisting of sodium bicarbonate, potassium bicarbonate, sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, calcium carbonate, calcium oxide and mixtures thereof.
14. The method according to claim 10 wherein the pH of the first composition ranges from 2.5 to 5.5.
15. The method according to claim 10 wherein the pH of the second composition ranges from 7.2 to 11.
16. The method according to claim 11 wherein the pH of the first composition results from inclusion of a compound selected from the group consisting of hydrogen peroxide, inorganic adds, C2-C20 carboxylic acids and mixtures thereof.
17. The method according to claim 11 wherein the monolithic combination of water soluble calcium salts are selected from the group consisting of calcium chloride, calcium citrate, calcium sulphate and calcium acetate and the respective phosphate salts are selected from the group consisting of sodium phosphate, ammonium phosphate and sodium ammonium phosphate.
18. The method according to claim 11 further comprising from about 0.01 to about 20% by weight of triclosan.
19. The method according to claim 11 further comprising from about 0.01 to about 20% by weight of a zinc salt.
Priority Applications (1)
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US09/538,564 US6248310B1 (en) | 1999-04-16 | 2000-03-29 | Anti-tartar dental product and method |
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Application Number | Priority Date | Filing Date | Title |
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US12977999P | 1999-04-16 | 1999-04-16 | |
US09/395,064 US6207139B1 (en) | 1999-04-16 | 1999-09-13 | Anti-tartar dental product and related method |
US09/538,564 US6248310B1 (en) | 1999-04-16 | 2000-03-29 | Anti-tartar dental product and method |
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US09/538,564 Expired - Lifetime US6248310B1 (en) | 1999-04-16 | 2000-03-29 | Anti-tartar dental product and method |
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US09/395,064 Expired - Lifetime US6207139B1 (en) | 1999-04-16 | 1999-09-13 | Anti-tartar dental product and related method |
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US (2) | US6207139B1 (en) |
EP (1) | EP1178773B1 (en) |
AT (1) | ATE302588T1 (en) |
AU (1) | AU3432600A (en) |
CA (1) | CA2365363A1 (en) |
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Also Published As
Publication number | Publication date |
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DE60022180D1 (en) | 2005-09-29 |
US6207139B1 (en) | 2001-03-27 |
WO2000062749A1 (en) | 2000-10-26 |
DE60022180T2 (en) | 2006-03-23 |
MXPA01010343A (en) | 2002-03-27 |
ES2248056T3 (en) | 2006-03-16 |
EP1178773B1 (en) | 2005-08-24 |
AU3432600A (en) | 2000-11-02 |
ATE302588T1 (en) | 2005-09-15 |
CA2365363A1 (en) | 2000-10-26 |
EP1178773A1 (en) | 2002-02-13 |
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